Chemical Structure : HM-279
CAS No.:
3039954-64-5
HM-279
(HM279)
Catalog No.: PC-24274Not For Human Use, Lab Use Only.
HM-279 is a potent, selective, orally bioavailable inhibitor of ALK5 (TGFβR1) with IC50 of 4.7 nM, strongly inhibits the phosphorylation of Smad3 in A549 cells (IC50=21.6 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HM-279 is a potent, selective, orally bioavailable inhibitor of ALK5 (TGFβR1) with IC50 of 4.7 nM, strongly inhibits the phosphorylation of Smad3 in A549 cells (IC50=21.6 nM).
HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5–693-fold selectivity.
HM-279 induces antitumor activity through modulation of antitumor immunity rather than direct cytotoxicity to cancer cells.
HM-279 (p.o., 30 mg/kg, QD antitumor activity of HM-279 in nude mice or a CD8+ T cell depletion mouse model.
Physicochemical Properties
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M.Wt
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451.55
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Formula
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C22H25N7O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((1-(But-2-yn-1-yl)-1H-pyrazol-4-yl)(cyclopropylmethyl)amino)-5-(4-(dimethylcarbamoyl)-1H-pyrrol-2-yl)thiazole-4-carboxamide
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References
1. Arai M, et al. J Med Chem. 2025 Mar 19. doi: 10.1021/acs.jmedchem.4c02293.
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